PMID: 11902797Mar 21, 2002Paper

Poly(L-lysine) as a model drug macromolecule with which to investigate secondary structure and membrane transport, part I: Physicochemical and stability studies

The Journal of Pharmacy and Pharmacology
Montakarn ChittchangThomas P Johnston

Abstract

Low oral bioavailability of therapeutic peptides and proteins generally results from their poor permeability through biological membranes and enzymatic degradation in the gastrointestinal tract. Since different secondary structures exhibit different physicochemical properties such as hydrophobicity, size and shape, changing the secondary structure of a therapeutic polypeptide may be another approach to increasing its membrane permeation. Poly(L-lysine) was used as a model polypeptide. The objectives of this study were to induce secondary structural changes in poly(L-lysine) and to determine the time course over which a given conformer was retained. In addition, the hydrophobicity of each secondary structure of poly(L-lysine) was assessed. The circular dichroism (CD) studies demonstrated that the conditions employed could successfully induce the desired secondary structural changes in poly(L-lysine). The alpha-helix conformer appeared to be more stable at 25 degrees C whereas the beta-sheet conformer could be preserved at 37 degrees C. On the other hand, the random coil conformer was retained at both temperatures. Significant losses of the alpha-helix and the beta-sheet conformers were observed when the pH was reduced. The chang...Continue Reading

References

Aug 1, 1978·Proceedings of the National Academy of Sciences of the United States of America·H J Ryser, W C Shen
Jul 1, 1979·Proceedings of the National Academy of Sciences of the United States of America·L J ArnoldN O Kaplan
Jan 1, 1991·Journal of Medicinal Chemistry·S H RosenbergW R Baker
Nov 1, 1990·Biomaterials·D Harris, J R Robinson
Feb 1, 1966·The Journal of Physical Chemistry·J Hermans
Apr 19, 1966·Biochemical and Biophysical Research Communications·B DavidsonG D Fasman
Dec 1, 1996·Journal of Pharmaceutical Sciences·P S BurtonR T Borchardt
Mar 11, 1998·International Journal of Biological Macromolecules·A I ArunkumarC Yu
Jun 6, 2000·Advanced Drug Delivery Reviews· T Borchardt RG M Pauletti

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Citations

Feb 13, 2016·The Journal of Physical Chemistry. B·Emma V YatesChristopher M Dobson
Nov 14, 2006·Journal of Molecular Biology·Raquel F EpandRichard M Epand
Feb 5, 2013·Acta Biomaterialia·M BinazadehL D Unsworth
May 20, 2009·Journal of Physics. Condensed Matter : an Institute of Physics Journal·F BordiD Truzzolillo
Dec 14, 2005·Journal of Biomedical Materials Research. Part a·Ijaz AhmedSally Meiners

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